1199266-76-6Relevant articles and documents
Kinetics and Mechanism of Bromination of 2-Pyridone and Related Derivatives in Aqueous Solution
Tee, Oswald S.,Paventi, Martino
, p. 4142 - 4146 (1982)
The tautomeric system 2-pyridone 2-hydroxypyridine (1a 2a) reacts with aqueous bromine via the principal tautomer 1a at pH 6.Attack upon 1a occurs preferentially at the 3 position, whereas reaction upon the anion probably involves major attack at the 5 position.The facile dibromination of 2-pyridone results from the comparable reactivity of the monobromopyridones at pH 4.These conclusions are based upon kinetic and product studies of the bromination of 1a and various derivatives in aqueous solutions at pH 0-8.With respect to their reactivity toward bromine the pyridones behave as substituted phenoxide ions.
A practical, laboratory-scale synthesis of Perampanel
McElhinny Jr., Charles J.,Carroll,Lewin, Anita H.
, p. 57 - 62 (2012)
The orally active, noncompetitive, selective AMPA receptor antagonist Perampanel, 2-[1,6-dihydro-6-oxo-1-phenyl-(2,3-bipyridin)-5-yl]benzonitrile, has been prepared from readily available, relatively inexpensive starting materials. The synthesis was carried out on a laboratory scale with no specialized equipment, and involved only two chromatographic purifications. Georg Thieme Verlag Stuttgart. New York.
Preparation method of ortho-alkoxy substituted pyridine compound
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Paragraph 0063-0064, (2021/09/08)
The invention provides a preparation method of an ortho-alkoxy substituted pyridine compound, the preparation method comprises the following step: reacting an ortho-amino substituted pyridine compound with an ortho-formate compound in the presence of a nitrite compound to generate the ortho-alkoxy substituted pyridine compound. The method has the advantages of high efficiency, low cost, environmental protection and the like.
COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY
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Paragraph 0088; 0096, (2020/04/09)
The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a PD-1 signaling inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and the PD-1 signaling inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a PD-1 signaling inhibitor and a pharmaceutically acceptable carrier or excipient.
COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY
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Page/Page column 26; 29, (2018/05/24)
The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a BCL-2 inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and a BCL-2 inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a BCL-2 inhibitor and a pharmaceutically acceptable carrier or excipient.
Preparation method of 2,5-dimethoxy pyridine
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Paragraph 0146; 0147; 0148; 0149, (2018/12/13)
The invention discloses a preparation method of 2,5-dimethoxy pyridine, and belongs to the technical field of medicine synthesis. The method comprises the following steps that 1, under the existence of an alcohol solvent, a compound shown as a formula A and sodium methoxide take contact reaction to form a compound shown as a formula B; 2, under the existence of metal catalysts, the compound shownas a formula B in the first step reacts to obtain 2,5-dimethoxy pyridine; aftertreatment and purification are performed to obtain the product. The method has the advantages that the route is short; the steps are few; expensive palladium catalysts and boracic acid catalysts are not used; the equipment cost is reduced; the use of flammable and explosive lithium reagents and peroxide is avoided; thereaction conditions are mild; the aftertreatment operation is simple and convenient; the total yield and the purity are improved; the product quality can be easily controlled; the industrial amplification prospects are good.
Reversible Folding of a β-Hairpin Peptide by a Metal-Chelating Amino Acid
Reutzel, Jan,Diogo, Timm M.,Geyer, Armin
supporting information, p. 8450 - 8456 (2017/06/28)
5-(1-Hydroxy-pyridin-2(1H)-onyl)-l-alanine (Hop) is a N-hydroxy-1,2-pyridone functionalized α-amino acid with the desired metal-chelating properties of DOPA (3,4-dihydroxy phenylalanine) but without its unwanted redox activity. The Fmoc-protected amino acid Fmoc-l-Hop(tBu)-OH (11) was synthesized from glycine phosphonate followed by enzymatic hydrolysis of the methyl ester yielding the Hop l-isomer in 96 % ee. The amino acid 11 is used in automated peptide synthesis for the assembly of a 14mer β-hairpin peptide with the sequence [dsb1, 14]H-CHXETGKHGHKLVC-OH (X=W, l-Hop). While the 10 π electron containing indole side chain of l-Trp in peptide 14 completes the formation of a hydrophobic cluster and results in 90 % folding, the folded fraction is significantly decreased to approximately 30 % for the 6 π electron l-Hop side chain in peptide 16. Metal chelation of Ga3+ reconstitutes the folding of 16 to above 60 % due to the formation of the Ga(16)3 trimer. The chelation process of 16 is monitored by NMR spectroscopy and the subsequent release of Ga3+ by a competitive metal chelator exemplifies the reversible oligomerization of peptide epitopes by metal chelation, bearing the opportunity to synthesize protein-sized aggregates on the basis of reversible chemistry in water.
Novel synthesis method for ortho-alkane superseded pyridine
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Paragraph 0018; 0019; 0020; 0021, (2017/07/19)
The invention relates to a novel synthesis method for ortho-alkane superseded pyridine. According to the method, ortho halogenated pyridine serves as raw materials, the ortho halogenated pyridine and corresponding alcohol react to obtain the ortho-alkane superseded pyridine under the action of sodium hydroxide. The reaction has universality for the ortho halogenated pyridine, and the method is simple and practical. Influence of consumption of the sodium hydroxide on mono-substitution and di-substitution in the reaction is inspected, alkoxy mono-substitution products and alkoxy di-substitution production are acquired, and a novel simply-operated, economical and favorable process for synthesis ortho-alkane superseded pyridine is provided.
COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE
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Page/Page column 21, (2016/10/11)
This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administrat
Phosphoinositide 3-kinase inhibitor with a zinc binding moiety
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Page/Page column 35, (2016/02/26)
The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
